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Medicinal Chemistry: Drug Synthesis and Optimization

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Medicinal Chemistry: Drug Synthesis and Optimization

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Questions and Answers

What is the primary goal of development synthesis in medicinal chemistry?

To synthesize a clinical candidate as efficiently and safely as possible (correct)

To identify the pharmacophore of a lead compound

To modify natural products with similar structural motifs

To synthesize lots of analogs as efficiently as possible

What approach involves identifying compounds with similar structures and modifying the synthetic route to apply to target compounds?

Convergent synthesis

Modification of natural products

Identification of compounds with similar structures (correct)

Retrosynthetic analysis

What is the advantage of convergent synthesis over linear synthesis?

It results in a higher overall yield (correct)

It results in a lower overall yield

It is more complex and difficult to design

It requires more starting materials

What is the primary consideration when selecting a synthetic route?

The yield and purity of the products Signup and view all the answers

What is the purpose of retrosynthetic analysis in medicinal chemistry?

To design a synthetic route for a target compound Signup and view all the answers

What is the goal of hit to lead optimization in medicinal chemistry?

To optimize a lead compound for pharmacodynamics and pharmacokinetics Signup and view all the answers

What is the main difference between MK-2 and CDK-2?

Their selectivity models Signup and view all the answers

What is the problem that was solved in the development of an analog-friendly route?

Incorporation of a chiral amine Signup and view all the answers

What is the role of BINAP in the synthesis of 2-Phenyl Pyridines?

A ligand for the palladium catalyst Signup and view all the answers

What is the purpose of the mCPBA step in the development of an analog-friendly route?

To form a sulfoxide bond Signup and view all the answers

What is the characteristic of the synthesis route described?

Scaleable synthesis with little/no chromatography Signup and view all the answers